During the last 20 years, obesity has become an increasingly common problem in the populations of developed countries. The increased incidence of obesity is partly due to the adoption of a westernised diet in many developed countries—which contains many foods with high fat and low fiber concentrations—and partly due to the lifestyle of westernized society. Obesity is known to increase the risk of contracting disorders such as diabetes, cardiovascular disease and hypertension.
Pharmacological approaches to the treatment of obesity either try to increase the body's energy expenditure, thereby burning more fat, or reduce the body's energy intake. The latter approach has stimulated the development of a variety of drugs which attempt to reduce the body's ability to absorb fat. These drugs target the enzymes responsible for the digestion of fat in the human digestive cycle. The most important enzymes in the digestion of fat are hydrolytic enzymes. The most significant of these enzymes are lipases, pancreatic lipase in particular. Orlistat, a derivative of lipstatin, a lipase inhibitor, is disclosed as an anti-obesity drug in European Patent Application No. EP129748. Other lipase inhibitors are disclosed in PCT International Publication Nos. WO 00/40569 and WO 00/40247, respectively.